| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
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| Other Sizes |
| Targets |
Halofantrine exerts its antimalarial effect by inhibiting heme polymerase, an enzyme used by the malaria parasite to detoxify heme. By inhibiting this enzyme, halofantrine causes the accumulation of toxic heme, leading to parasite death. It is also a blocker of the delayed rectifier potassium current via inhibition of the human ether-a-go-go-related gene (hERG) channel. Halofantrine has been shown to preferentially block open and inactivated hERG channels, which contributes to some degree of cardiotoxicity.
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| ln Vitro |
In vitro, halofantrine demonstrates potent antimalarial activity against P. falciparum. Its activity is typically assessed using [³H]hypoxanthine incorporation assays, with IC₅₀ values in the low nanomolar range. Halofantrine is active against both chloroquine-sensitive and chloroquine-resistant strains. It also shows activity against multidrug-resistant strains, including those resistant to mefloquine. In vitro susceptibility testing uses final concentrations ranging from 0.25 to 32 nM for halofantrine.
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| ln Vivo |
In vivo, halofantrine has demonstrated efficacy in animal models of malaria. It has been studied for its pharmacokinetics, efficacy, and toxicity in uncomplicated malaria. The compound is effective as a blood schizonticide against malaria parasites. However, its clinical use is limited by its cardiotoxic effects related to hERG channel blockade. In vivo pharmacogenetic studies have shown that the metabolism of halofantrine may be modulated by genetically determined polymorphic CYP2D6 activity.
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| Enzyme Assay |
In vitro enzyme assays for halofantrine typically measure its inhibition of heme polymerase activity. The assay involves incubating the parasite enzyme with heme substrate and varying concentrations of halofantrine. The amount of heme polymerization is measured spectrophotometrically. For hERG channel studies, patch-clamp electrophysiology is used to assess the compound's effects on potassium currents in cells expressing the hERG channel.
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| Cell Assay |
In vitro cellular assays for halofantrine use P. falciparum cultures to assess antimalarial activity. The standard microdilution radioisotope method involves culturing parasites in 96-well plates with various concentrations of halofantrine. [³H]hypoxanthine is added, and its incorporation into parasite nucleic acids is measured to determine parasite viability. IC₅₀ values are calculated from dose-response curves. The compound is tested against both chloroquine-sensitive and chloroquine-resistant strains.
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| Animal Protocol |
In vivo animal studies for halofantrine typically involve mouse models of malaria infection. Mice are infected with P. falciparum or P. berghei and then treated with halofantrine via various routes of administration. Parasitemia is monitored by blood smears, and the compound's efficacy is assessed by reduction in parasitemia and survival rates. Pharmacokinetic studies in animals involve administering the compound and measuring plasma concentrations over time.
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| ADME/Pharmacokinetics |
Halofantrine hydrochloride has a molecular formula of C₂₆H₃₁Cl₃F₃NO and a molecular weight of 536.88. It is typically stored as a powder at -20°C for up to 3 years and in solution at -80°C for 6 months. The compound is a blocker of the delayed rectifier potassium current via inhibition of the hERG channel. Its pharmacokinetic profile includes oral absorption, with metabolism primarily mediated by CYP2D6.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation Since there is currently no information regarding the use of halofantraline during lactation, it is recommended to prioritize other medications, especially when breastfeeding newborns or premature infants. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found. ◉ Effects on Lactation and Breast Milk As of the revision date, no relevant published information was found. |
| References | |
| Additional Infomation |
A stereospecific liquid chromatographic (LC) assay has been developed for the quantification of halofantrine enantiomers in human plasma. The compound is an antimalarial drug with demonstrated activity against P. falciparum. It is for research use only and has not been fully validated for medical applications. The compound's cardiotoxicity is related to its hERG channel blocking activity. Halofantrine is structurally related to other antimalarials such as mefloquine and lumefantrine.
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| Molecular Formula |
C26H31CL3F3NO
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|---|---|
| Molecular Weight |
536.88
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| Exact Mass |
535.142
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| CAS # |
36167-63-2
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| Related CAS # |
Halofantrine;69756-53-2
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| PubChem CID |
37392
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| Appearance |
White to off-white solid powder
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| Density |
1.244g/cm3
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| Boiling Point |
596.2ºC at 760mmHg
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| Flash Point |
314.4ºC
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| LogP |
9.446
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
34
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| Complexity |
584
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WANGFTDWOFGECH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H30Cl2F3NO.ClH/c1-3-5-10-32(11-6-4-2)12-9-25(33)23-16-22-21(14-18(27)15-24(22)28)20-13-17(26(29,30)31)7-8-19(20)23;/h7-8,13-16,25,33H,3-6,9-12H2,1-2H3;1H
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| Chemical Name |
3-(dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)phenanthren-9-yl]propan-1-ol;hydrochloride
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| Synonyms |
Halofantrine HCl; Halfan; Halofantrine hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~30 mg/mL (~55.88 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8626 mL | 9.3131 mL | 18.6261 mL | |
| 5 mM | 0.3725 mL | 1.8626 mL | 3.7252 mL | |
| 10 mM | 0.1863 mL | 0.9313 mL | 1.8626 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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